CYP1A2 is the major isoform responsible for paeonol O-demethylation in human liver microsomes

被引：18

作者：

Liu, H. -X. ^{[1
,2
]}

Hu, Y. ^{[1
]}

Liu, Y. ^{[1
]}

He, Y. -Q. ^{[3
]}

Li, W. ^{[1
,2
]}

Yang, L. ^{[1
]}

机构：

[1] Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China

[2] Chinese Acad Sci, Grad Sch, Beijing, Peoples R China

[3] Shanghai Univ Tradit Chinese Med, Shanghai, Peoples R China

来源：

XENOBIOTICA | 2009年 / 39卷 / 09期

关键词：

Paeonol; cytochrome P450; O-demethylated metabolite; NF-KAPPA-B; CYTOCHROME-P450; METABOLISM; EXPRESSION; INDUCTION; ENZYMES; POLYMORPHISM; VARIABILITY; INHIBITION; MECHANISM;

D O I：

10.1080/00498250902998681

中图分类号：

R9 [药学];

学科分类号：

100702 [药剂学];

摘要：

1. Paeonol, the primary active component of a traditional Chinese medicine Moutan Cortex, has a wide range of pharmacological activities. In the present study, the metabolism of paeonol by cytochrome P450s (CYPs) was investigated in human liver microsomes. 2. One O-demethylated metabolite was detected in reaction catalysed by human liver microsomes, and was identified as resacetophenone by comparing the tandem mass spectra and the chromatographic retention time with that of the standard compound. 3. The study with a chemical selective inhibitor, cDNA-expressed human CYPs, a correlation assay, and a kinetics study demonstrated that CYP1A2 was the major isoform responsible for the paeonol O-demethylation in human liver microsomes.

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收藏

页码：672 / 679

页数：8

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